Choludexan - instructions for use, dose, side effects, contraindications

Excipients - corn starch (granulated) - 10,364 mg, corn starch - 66,016 mg (including additional 4,00 mg for moisture compensation), silicon dioxide colloid (aerosil 200) - 5.50 mg, magnesium stearate 2.0 mg, potassium sorbate - 0.34245 mg;

gelatin capsule composition: gelatin - 96,254 mg, titanium dioxide - 1,585 mg, dye azorubin - 0,116 mg, dye crimson [Ponso 4R] (for lid only) - 0.044 mg.

Description:Hard gelatin capsules in size 0, the case is pink, the lid is red. Capsule contents - granular powder balogo or almost white color.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

Holudexan - hepatoprotective agent, also has choleretic, cholelitolitic, hypolipidemic, hypocholesterolemic and some immunomodulating action.

Possessing high polar properties, ursodeoxycholic acid (UDCA) forms a non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of the gastric reflyuktata damaging cell membranes at a biliary reflux gastritis and reflux-esophagitis. In addition, UDCA forms double molecules that can be incorporated into cell membranes (hepatocytes, cholangiocytes, epitheliocytes of the digestive tract (gastrointestinal tract)), stabilize them and do not be immune to the action of cytotoxic micelles. Reducing the concentration of toxic to the hepatic cell bile acids and stimulating choleresis, rich in bicarbonates, UDCA effectively contributes to the resolution of intrahepatic cholestasis. It decreases the saturation of bile with cholesterol by inhibiting its absorption in the intestine, suppression of hepatic synthesis and decreasing secretion in bile; increases the solubility of cholesterol in bile, forming with it liquid crystals; reduces lithogenic bile index. The result is the dissolution of cholesterol bile stones and the prevention of the formation of new concrements. Immunostimulating effect due to inhibition of expression of antigens HLA-1 on membranes of hepatocytes and HLA-2 on cholangiocytes, by the normalization of the natural killer activity of lymphocytes, etc. Reliably delays progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic stoatohepatitis; reduces the risk of developing varicose veins of the esophagus. UDCA slows down the processes of premature aging and cell death (hepatocytes, cholangiocytes, etc.).

Pharmacokinetics:

UDCA is absorbed in the small intestine due to passive diffusion (about 90%), and in the ileum through active transport. The maximum concentration in the blood plasma (C_m_Oh) when administered orally 50 mg after 30, 60, 90 minutes, 3.8 mmol / L, 5.5 mmol / L and 3.7 mmol / L, respectively. FROM_m_Oh is achieved in 1-3 hours. The connection with proteins is high - up to 96-99%. Penetrates through the placental barrier. With the systematic administration of cholodexane, UDCA becomes the main bile acid in the blood serum and accounts for about 48% of the total amount of bile acids in the blood. The therapeutic effect of the drug depends on the concentration of UDCA in the bile.

Metabolised in the liver (clearance during primary passage through the liver) into taurine and glycine conjugates.The resulting conjugates are secreted in bile. About 50-70% of the total dose of the drug is excreted by bile. A small amount of unsweetened UDCA enters the large intestine, where it undergoes cleavage by bacteria (7-dehydroxylation); the resulting lithocholic acid is partially absorbed from the colon but is sulfated in the liver and is rapidly excreted as a sulfolithocholylglycine or sulfolithocholyltaurine conjugate.

Indications:

Uncomplicated cholelithiasis (biliary sludge, dissolution of cholesterol gallstones in the gallbladder if they can not be removed by surgical or endoscopic methods, prevention of recurrence of stone formation after cholecystectomy)

Chronic active hepatitis

Toxic (including medicinal) liver damage

Alcoholic liver disease (ABP)

Non-alcoholic steatohepatitis

Primary biliary cirrhosis of the liver

Primary sclerosing cholangitis

Cystic Fibrosis

Atresia of the intrahepatic biliary tract, congenital atresia of the bile duct

Dyskinesia of the biliary tract

Biliary reflux gastritis and reflux esophagitis

Contraindications:

Hypersensitivity to the drug, X-ray positive (high in calcium) gallstones, a dysfunctional gallbladder, cholecystitis, acute cholecystitis, acute cholangitis, cirrhosis of the liver in the stage of decompensation, acute infectious diseases of the gallbladder, bile ducts and intestines, marked hepatic and / or renal failure, obstruction of the bile ducts, empyema of the gallbladder, children under 3 years.

Carefully:

Although UDCA does not have age limitations in use, use Holudexan capsules with caution in children between the ages of 3 and 4 years. possible difficulty in swallowing capsules.

Pregnancy and lactation:

Women of childbearing age during the period of drug use are advised to use non-hormonal contraceptives. The use of UDCA in pregnancy is possible only if the expected benefit for the mother exceeds the potential risk for the fetus (adequate strictly controlled studies of the use of UDCA in pregnant women have not been conducted). Data on the isolation of UDCA with breast milk are currently not available.If UDCA is necessary in the lactation period, the question of stopping breastfeeding should be addressed.

Dosing and Administration:

Choludexan is taken orally, with a sufficient amount of water, with biliary reflux gastritis and reflux esophagitis - 1 once a day, before bed, with diffuse liver diseases - 2-3 times a day with food.

Chronic liver disease; cholelithiasis (cholesterol gallstones and biliary sludge) - continuously for a long time (from several months to several years) in a daily dose of 10 mg / kg to 12-15 mg / kg (2-5 capsules). Duration of admission for dissolution of stones - until complete dissolution, plus 3 more months to prevent recurrence of stone formation.

With biliary reflux gastritis and reflux esophagitis - 300 mg (1 capsule) per day, before bedtime. The course of treatment is from 10-14 days to 6 months, if necessary up to 2 years.

After cholecystectomy, for prevention of recurrent cholelithiasis, 300 mg 2 once a day for several months.

Toxic, medicinal liver damage, ABP and atresia of the biliary tract - 10-15 mg / kg / day for 6-12 months or more.

Primary biliary cirrhosis - 10-15 mg / kg / day (if necessary - up to 20 mg / kg) from 6 months to several years.

Primary sclerosing cholangitis is 12-15 mg / kg / day (up to 20 mg / kg) from 6 months to several years.

Nonalcoholic steatohepatitis - 13-15 mg / kg / day from 6 months to severalyears.

Cystic fibrosis - 20-30 mg / kg / day (up to 20 mg / kg) from 6 months to several years.

Children older than 3 years UDHK appoint individually, based on 10-20 mg / kg / day.

Side effects:

Back pain, nausea, vomiting, diarrhea (can be dose-dependent), constipation, transient (transient) increase in the activity of "liver" transaminases, allergic reactions; rarely - calcification of gallstones, exacerbation of previously existing psoriasis, alopecia.

Overdose:Cases of overdose UDCA are not known.

Interaction:Antacids containing aluminum and ion-exchange resins (colestramine), reduce the absorption of the drug. Lipid-lowering drugs (especially clofibrate), estrogens, neomycin or progestins increase bile saturation with cholesterol and may decrease the ability to dissolve cholesterol bile stones. Increases the effect of oral hypoglycemic drugs.

Special instructions:

Pediatric Use

Since it may be difficult to swallow the capsules, the drug should not be used in this dosage form in children under 3 years of age; in children from 3 to 4 years of age is used with caution.

When taking the drug for the purpose of dissolution of gallstones, it is necessary to observe the following conditions: the stones should be cholesterol (X-ray negative), their size should not exceed 15-20 mm, the gallbladder should remain functional and should be filled with stones no more than half, and the common bile duct should be preserved. With prolonged (more than 1 month) taking the drug every 4 weeks in the first 3 months of treatment, in the future - every. 3 month to conduct a biochemical blood test to determine the activity of "liver" transaminases. Control of treatment effectiveness should be carried out every 6 months according to ultrasound and radiographic examination of bile ducts. After complete dissolution of the stones, it is recommended that the use of Choludexan be continued for at least 3 months in order to facilitate the dissolution of stone remains that are too small for their detection to prevent the recurrence of stone formation.

If within 6 months after the beginning of therapy of partial dissolution of stones did not occur, it is unlikely that the treatment will be effective.

Effect on the ability to drive transp. cf. and fur:

The drug does not adversely affect the ability to drive vehicles and / or other mechanisms.

Form release / dosage:

Capsules 300 mg.

Packaging:

10 capsules in a blister of aluminum foil and polyvinyl chloride film.

2 or 6 blisters are placed in a cardboard box together with an instruction for use.

Storage conditions:

Store at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:PL-000723

Date of registration:29.09.2011 / 05.08.2014

Expiration Date:29.09.2016

The owner of the registration certificate:World Medical Co., Ltd.World Medical Co., Ltd. Egypt

Manufacturer: & nbsp

Sigma Pharmaceutical Industries Egypt

Representation: & nbspTROKAS PHARMA LLCTROKAS PHARMA LLCRussia

Information update date: & nbsp12.07.2016

Illustrated instructions

Instructions

Holudexan (Choludexan)